THREE INDEPENDENT SERVICE MODULES
Discovery of Candidates
Employ Micro-Tag™ platform to discover novel unbiased drug candidates:
- DNA-Encoded Libraries (DELs) - We can support any DEL library of choice carrying various chemistries, including covalent and non-covalent ligands. DEL data can be directly used for testing of promising candidates. Alternatively, DEL data can be further enhanced using AI/ML analysis.
- Plated libraries - We can work with plated libraries of any size, ranging from tens / hundreds to thousands of candidates. Once the assay is developed for the target of interest, throughput can be optimized and scaled. Promising candidates can be grouped and re-evaluated.
Validation & Ranking
Selected drug candidates can be further prioritized to guide medicinal chemistry and accelerate decision making:
- Ranking of candidates by potency of target engagement - Any number of selected candidates can be ranked by their EC50 values. Several different temperatures of aggregation (T-agg) of the target can be tested for accurate selection of potent binders. Both target stabilizers and de-stabilizers will be identified and classified by potency. Ranking is independent of therapeutic modality.
- Validation of target selectivity - Selected candidates can in parallel be tested against control targets, within target's class and / or other unrelated targets. Target selectivity profile is important for assessment of clinical potential.
Analysis and MoA
Mechanistic insight for your most promising candidates can be gained directly in the cell accelerating path to lead optimization:
- Real-time analysis of cell target engagement - This will provide kinetic assessment for the selected drug-target pairs. Association rates (K-on), binding affinities (KD) and target saturating doses (E-max) can be measured in real-time.
- Real-time live cell imaging - This will enable imaging and measurement of target abundance in response to the selected ligand. This application is ideally suited for target degraders.